Fungicidal composition for treating the human skin



Patented Dec. 4, 1951 FUNGI'CIDAL COMPOSITION FOR. TREATING THE HUMAN SKIN James A. Wyman, Arlington, Va.

No Drawing. Application July 8, 1948, Serial No. 37,517

5 Claims. l

My invention is a new composition of matter consisting of benzoin, a volatile solvent and other compatible soluble fungicidal drugs and chernicals adapted for the treatment of fungus in fections. of the skin, scalp and hair and diseases resulting therefrom and other skin infections, diseases and irritations which frequently have the characteristic of responding tothe same type of treatment as mycotic skin diseases. These various skin diseases include microsporosis, trichophytosis, tinea capita, tineabarbae, tinea cruris,

tinea versicolor, various forms of eczema, favus,

gruitus, impetigo, and other similar skin infecons.

Skin infections and skin diseases of lower animals similar to the foregoing frequently respond to treatment by these compounds.

Heretofore various preparations have been used for the treatment of the foregoing skin conditions but such preparations frequently have proven unsatisfactory. Dissatisfaction may have resulted from failure of the therapeutic agent to reach the seat of the infection and there contact the offending organisms or because of obnoxious physical properties or effects. When a. compound has an oily or fatty base, the oils or fats tend to form envelopes around the therapeutic agents contained in such preparations and thus prevent effective contact with offending organisms. Also, such preparations frequently are unpleasant and obnoxious because of the greasy skin sensations produced thereby, or because of the bandaging required, or because of the adhesion of dirt, dust or other foreign matter to such compounds or bandages, or because of the smears and stains left by such preparations on the skin and clothing.

Further, some of the medications heretofore used for the treatment of skin diseases were unsatisfactory because certain ingredients were inscluble or not stably soluble in the composition, with resultant immediate or delayed precipitation or reversion. Such characteristics may indicate lack of inhibitive and penetrative powers.

The compounds comprising the present invention do not contain fats or oils, they thoroughly wet the secretions of diseased tissue, and they possess excellent powers of penetration and inhibition. Hence, the compounds of the present invention are free from the aforementioned obicctions which stem. from the inclusion of fatty orinsoluble ingredients in the medicament.

Distinguishing characteristics of the compounds within the purview of the. present inventionv are the complete solubility of, the ingredients and the stability of the liquid cornpounds thus formed. The penetrative power of the liquid base of these compounds enables the therapeutic agents in solution to penetrate into the seat of the infection and to some extent into the fatty tissues andthere inhibit the growth of the offending organism.

Another desirable characteristic of these compounds when used in treating skin diseases is their'power to curb or stop for extended periods the burning and itching sensations which freouently accompany such infections. This characteristic is especially beneficial in the. treatment of childrens skin infections.

When applied to an infected area the volatile solvent in these compounds quickly evaporates leaving a light amber-colored medicated film or coating. Subsequent applications dissolve the film or coatin remaining from the previous ap-' plication and thus fresh, effective components of the compound are enabled intimately to contact and penetrate into the infected area and inhibit the growth or spread of the offending organism. The film is tenaciously adhesive and is not easily rubbed off, even when soap and water are used. The under side of the film or coating is miscible with the exudations and secretions of the infected area, and thus the effective ingredients in the medication are continuously in intimate contact with the offending organisms contained in and lying under such exudations and secretions.

Clinical experience has indicated that many organisms become tolerant of a specific fungicide before. the organisms are inhibited but that with a change in the medication the infection is cured without undue delay. The present invention lends itself perfectly to the incorporation of dif ferent fungicides, or combinations thereof, selected according to the art, to form thev different special compounds for the treatment of specific skin diseases.

The. desirable pharmacological properties of the individual ingredients incorporated in the compositions within the purview of this invention are not lessened when combined in these new compounds. On the contrary, the pharmacological properties of the ingredients when so incorporated are increased, improved and strengthened. Thus, this invention provides. a new combination of medicaments for the treatment of skin conditions.

In preparing these, compounds for the treat ment of skin diseases, the selected primary fungicidal agent, should bev dissolved, in tincture of benzoin. U. S. P., or if an additional volatile solvent is to be used, dissolve such agent in a base consisting of tincture of benzoin, U. S. P. and the added volatile solvent. Some of the fungicidal drugs and chemicals dissolve slowly, depending to some extent upon temperature, frequency of agitation, and other factors, taking up to forty-eight hours as, for example, in the case of salicylanilide under certain conditions. Continuous or frequent agitation will insure complete solution of the drugs or chemicals more quickly. Those skilled in the art will vary the percentage of the primary agents, or combinations thereof, to produce a weak, medium or strong composition depending upon the nature and location of the infection, the extent of the irritation, the condition of the infected skin and tissue, and other pertinent factors.

When a reduction in the proportion of benzoin is desired, a sufficient quantity of ethyl or isopropyl alcohol or acetone or similar compatible solvent may be added to the tincture of benzoin, U. S. P., to obtain the desired proportion of benzoin. When a greater proportion of benzoin is desired than is contained in tincture of benzoin, U. S. P. a predetermined percentage of gum of benzoin may be processed and dissolved according to the art to obtain the desired proportion of benzoin in the composition. However, for ordinary use in the treatment of skin diseases, tincture of benzoin, U. S. P. contains suficient benzoin for all practical purposes, even when up to 65% of a compatible volatile solvent is added to the tincture of benzoin, U. S. P.

It is mandatory to incorporate benzoin or an equivalent in the compounds within the purview of this invention.

For the treatment of the skin, the following ingredients or equivalents are used according to the art, within the indicated approximate percentages in the practice of this invention:

For a liquid base Name: Percentage Benzoin -40 Ethyl alcohol -85 Isopropyl 10-65 Acetone 10-65 To the foregoing liquid base is added one or more of the following primary fungicidal agents, or equivalents, within the prescribed approximate percentages:

Although not beyond doubt, the penetrative power of the compounds might be somewhat increased by the addition of from 1% to 5% of a compatible detergent. However, a detergent is believed to be unnecessary ordinarily when isopropyl alcohol or acetone are used, because being defatting agents the effective ingredients in the compound in solution are enabled by the action of such solvents to penetrate fatty tissues within the infected area.

.Those skilled in the art may easily provide "equivalents for the drugs and chemicals listed herein, within appropriate percentages, and the present invention is directed to theuse accordfng to the art of such equivalents.

4 While there is disclosed herein only ethyl alcohol and isopropyl alcohol and acetone as suitable solvents, other known volatile solvents could be used alone or in combinations according to the art so long as they are compatible with the other ingredients. Similarly, while the specific examples herein given are each limited to one primary fungicidal agent, except in Examples Nos. 2 and 3, combinations of two or more of the primary fungicidal agents listed herein, or equivalents, may be used according to the art in preparing these compounds so long as they are compatible with each other and with the other ingredients.

Those skilled in the art are cognizant of the hazards in using pentachlorphenol in the treatment of the skin because of its toxicity.

Examples of the preferred proportions of ingredients for combining according to the art in different special compounds for the treatment of skin diseases are as follows:

Example No. 1

Tincture of benzoin, U. S. P cc 70 Salicylanilide, C. P grams 4 Isopropyl alcohol q. s cc Example No. 2

Tincture of benzoin, U. S. P cc 70 Copper undecylenate, C. P gram 1 Undecylenic acid, C. P grams 5 Acetone q. s cc 100 Example No. 3

Tincture of benzoin, U. S. P cc '70 Zinc undecylenate, C. P gram 1 Undecylenic acid grams 5 Acetone q. s cc 100 Example No. 4

Tincture of benzoin, U. S. P cc 70 Pentachlorphenol, tech "gram" 1 Isopropyl alcohol q. s cc 100 Example No. 5

Tincture of benzoin, U. S. P cc '70 Gentian violet, C. P grams" 2 Acetone q. s cc 100 Example No. 6

Tincture of benzoin, U. S. P l cc 70 Undecylenic acid, C. P grams 10 Isopropyl alcohol q. s cc 100 Example No. 7

Tincture of benzoin, U. S. P cc 70 Propionic acid, C. P grams (00.) l0 Isopropyl alcohol q. s cc 100 Example No. 8

Tincture of benzoin, U. S. P cc 70 Caprylic acid, C. P grams (cc.) 10 Isopropyl alcohol q. s cc 100 Example No. 9

Tincture of benzoin, U. S. P cc '70 Salicylic acid, C. P grams .5 Isopropyl alcohol q. s cc 100 To reduce the hazard of deterioration of the ingredients in these compounds colored glass containers are preferred.

The liquid composition may be applied on the area to be treated by any kind 'or type of applicator but a cotton-tipped stick-type applicator, ordinarily to be discarded after initial; use, is preferred. The applicator should be designed to take up a small quantity of the composition to form a thin film or coating. In the treatment of skin diseases, the liquid should be applied on and approximately one-half inch beyond the infected area.

The compounds within the purview of the present invention for the treatment of the skin are fast drying stable liquids, easily applied, and when the volatile solvent evaporates there is formed a firm, tough, non-greasy, tenaciously adhesive effective medicated film or coating. The

. compounds for the treatment of skin diseases Tincture of benzoin, U. S. P. cc 70 Salicylanilide, C. P grams 4 Isopropyl alcohol q. s cc 100 said coating composition being adapted, upon application to the skin, to form a non-tacky flexible coating having said salicylanilide homogeneously dispersed therein and from which coating said silicylanilide is gradually released to act upon the infected area of the skin.

2. A permanently stable, homogeneous, substantially anhydrous, fungicidal liquid coating composition for the treatment of the skin consisting of Tincture of benzoin, U. S. P cc 70 Undecylenic acid, C. P grams Isopropyl alcohol q. s cc 100 said coating composition being adapted, upon application to the skin, to form a non-tacky flexible coating having said undecylenic acid homogeneously dispersed therein and from which coating said undecylenic acid is gradually released to act upon the infected area of the skin.

3. A permanently stable, homogeneous, substantially anhydrous, fungicidal liquid coating composition for the treatment of the skin consisting of Tincture of benzoin, U. S. P cc 70 Propionic acid, C. P grams (cc.) 10 Isopropyl alcohol q. s cc 100 said coating composition being adapted, upon application to the skin to form a non-tacky flexible coating having said propionic acid homogeneously dispersed therein and from which coating said propionic acid is gradually released to act upon the infected area of the skin.

4. A permanently stable, homogeneous, substantially anhydrous, fungicidal liquid coating composition for the treatment of the skin consisting of from 10-40 per cent benzoin as a film forming base; a volatile solvent selected from the A Book Co'., 1936, New York, page 300.

group consisting of ethyl alcohol 35-85 per cent, isopropyl alcohol 10-65 per cent, acetone 10-65 per cent and mixtures thereof with one another; and a fungicidal agent compatible in said solution with said benzoin selected from the group consisting of salicylanilide about 4 per cent, caprylic acid about 10 per cent, undecylenic acid about 10 per cent and propionic acid about 10 per cent and mixtures thereof with one another; said fungicidal agent being present in an amount normally irritating to the skin but which in said solution provides a saturated permanently compatible fungicidally-active solution of said agent which is non-irritating to the skin; said coating composition being adapted, upon application to the skin, to form a non-tacky flexible coating wherein said fungicidal agent is homogeneously dispersed and from which coating said agent is gradually released to act upon the infected area of the skin.

5. A permanently stable, homogenous, substantially anhydrous liquid coating composition for the treatment of the skin consisting of:

Tincture of benzoin, U. S. P cc '70 Caprylic acid, C. P grams (cc.) 10 Isopropyl alcohol q. s cc said coating composition being adapted, upon application to the skin, to form a non-tacky flexible coating having said caprylic acid homogeneously dispersed therein and from which coating said caprylic acid is gradually released to act upon the infected area of the skin.

JAMES A. WYMAN.

'REFERENCES CITED The following references are of record in the file of this patent:

UNITED STATES PATENTS Number Name Date 1,582,912 Ellis May 4, 1926 1,924,169 Stacey Aug. 29, 1933 OTHER REFERENCES Grottewit, Med. Record, Jan. 18, 1939, pages 313-315. 167-5812.

Hudgins, The West Virginia Medical J., Feb. 1930, page 82. 167-5812 Sutton, Diseases of the Skin, 10th ed., C. V. Mosby Co., St. Louis, 1939, page 1082. (Copy in Division 43.)

Grant, Am. Jour. Pharm, June 1922, pages 421-422. 167-9 1. (Copy in P. O. S. L.)

Goodman, Cosmetic Dermatology, McGraw Hill (Copy in Division 43.)

Schwartz, Am. J. Pharmacy, Jan. 1947, pages 5-14. (Copy in 167-58R.)

Pharmaceutical Formulas, 11th ed. 1944, Chemist and Druggist, London, vol. I, page 706. (Copy in Division 43.)

Lesser, Drug and Cosmetic Industry, Sept. 1943, pages 272, 273.

MacArthur, Clinical Medicine, Oct. 1941, page 259. 167-581? Revista Farmaceutica, 1936, page 441. 167-58. 

1. A PERMANENTLY STABLE, HOMOGENOUS, SUBSTANTIALLY ANHYDROUS, FUNGICIDAL LIQUID COATING COMPOSITION FOR THE TREATMENT OF THE SKIN CONSISTING OF: 